scholarly journals APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
V. C. Karade ◽  
A. Sharma ◽  
R. P. Dhavale ◽  
R. P. Dhavale ◽  
S. R. Shingte ◽  
...  
Keyword(s):  
Controlled Release ◽  
Photoelectron Spectroscopy ◽  
Superparamagnetic Iron Oxide ◽  
In Vitro Cytotoxicity ◽  
Human Lung Cancer ◽  
Prolonged Release ◽  
Magnetic Nanospheres ◽  
Self Assembled ◽  
Monolayer Coverage

AbstractThe use of an appropriate delivery system capable of protecting, translocating, and selectively releasing therapeutic moieties to desired sites can promote the efficacy of an active compound. In this work, we have developed a nanoformulation which preserves its magnetization to load a model anticancerous drug and to explore the controlled release of the drug in a cancerous environment. For the preparation of the nanoformulation, self-assembled magnetic nanospheres (MNS) made of superparamagnetic iron oxide nanoparticles were grafted with a monolayer of (3-aminopropyl)triethoxysilane (APTES). A direct functionalization strategy was used to avoid the loss of the MNS magnetization. The successful preparation of the nanoformulation was validated by structural, microstructural, and magnetic investigations. X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR) were used to establish the presence of APTES on the MNS surface. The amine content quantified by a ninhydrin assay revealed the monolayer coverage of APTES over MNS. The monolayer coverage of APTES reduced only negligibly the saturation magnetization from 77 emu/g (for MNS) to 74 emu/g (for MNS-APTES). Detailed investigations of the thermoremanent magnetization were carried out to assess the superparamagnetism in the MNS. To make the nanoformulation pH-responsive, the anticancerous drug Nintedanib (NTD) was conjugated with MNS-APTES through the acid liable imine bond. At pH 5.5, which mimics a cancerous environment, a controlled release of 85% in 48 h was observed. On the other hand, prolonged release of NTD was found at physiological conditions (i.e., pH 7.4). In vitro cytotoxicity study showed dose-dependent activity of MNS-APTES-NTD for human lung cancer cells L-132. About 75% reduction in cellular viability for a 100 μg/mL concentration of nanoformulation was observed. The nanoformulation designed using MNS and monolayer coverage of APTES has potential in cancer therapy as well as in other nanobiological applications.

N-Acetylserotonin vs Melatonin: In-Vitro Controlled Release from Hydrophilic Matrix Tablets

2019 ◽  
Vol 16 (3) ◽  
pp. 347-352 ◽  
Author(s):  
M. Vlachou ◽  
G. Stavrou ◽  
A. Siamidi ◽  
S. Flitouri ◽  
V. Ioannidou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Selective Serotonin Reuptake Inhibitors ◽  
Sleep Onset ◽  
Matrix Tablets ◽  
Melatonin Receptors ◽  
Solid Matrix ◽  
Poor Sleep ◽  
Prolonged Release ◽  
Hydrophilic Matrix

Background: N-Acetylserotonin (NAS, N-acetyl-5-hydroxytryptamine) is the immediate precursor of the neurohormone melatonin (MT, N-acetyl-5-methoxytryptamine), which regulates sleep and wake cycles. NAS is produced by the N-acetylation of serotonin and is converted to melatonin via the action of Acetylserotonin O-methyltransferase (ASMT). Like melatonin, NAS acts as an agonist on the melatonin receptors MT1, MT2, and MT3. However, as NAS is abundant in specific brain areas, separate from serotonin and melatonin, it may also have discrete central effects. Indicatively, it has been reported that NAS may play a role in the antidepressant effects of Selective Serotonin Reuptake Inhibitors (SSRIs) and Monoamine Oxidase Inhibitors (MAOIs). </P><P> Objective: To decipher the controlled release characteristics of the active substances (NAS and MT) in a quick initial pace, aiming at a satisfactory sleep-onset related anti-depressive profile and prolonged release, thereafter, targeting at coping with poor sleep quality problems. </P><P> Methods: A series of hydrophilic matrix tablets involving as excipients, hydroxypropylmethylcellulose (HPMC) K15M, low viscosity sodium alginate, lactose monohydrate, and polyvinylpyrrolidone (PVP) M.W.: 10.000 and 55.000) was developed and tested at two dissolution media (pH 1.2 and 7.4). </P><P> Results: The results showed that commonly used excipients with different physicochemical properties govern the controlled release of NAS and MT from solid matrix systems. </P><P> Conclusions: We have demonstrated how broadly used excipients affect the in vitro controlled release of NAS and MT from solid pharmaceutical formulations. Currently, we extend our studies on the controlled release of these drugs using various other biopolymers/formulants of different physicochemical characteristics, which will help to highlight the discrete release profiles of NAS and MT.

scholarly journals Synthesis, characterization and in vitro cytotoxicity study of Co and Ni ferrite nanoparticles prepared by sol-gel method

2021 ◽  
Vol 3 (7) ◽  
Author(s):  
Alexandre Pancotti ◽  
Dener Pereira Santos ◽  
Dielly Oliveira Morais ◽  
Mauro Vinícius de Barros Souza ◽  
Débora R. Lima ◽  
...  
Keyword(s):  
Photoelectron Spectroscopy ◽  
Sol Gel ◽  
Test Sample ◽  
In Vitro Cytotoxicity ◽  
Gel Method ◽  
X Ray ◽  
Sol Gel Method ◽  
Transmission Electron ◽  
Crystallite Sizes

AbstractIn this study, we report the synthesis and characterization of NiFe2O4 and CoFe2O4 nanoparticles (NPs) which are widely used in the biomedical area. There is still limited knowledge how the properties of these materials are influenced by different chemical routes. In this work, we investigated the effect of heat treatment over cytotoxicity of cobalt and niquel ferrites NPs synthesized by sol-gel method. Then the samples were studied using transmission electron microscopy (TEM), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), vibrating sample magnetometer (VSM), Fourier Transform Infrared Spectroscopy Analysis (FTIR), and X-ray fluorescence (XRF). The average crystallite sizes of the particles were found to be in the range of 20–35 nm. The hemocompatibility (erythrocytes and leukocytes) was checked. Cytotoxicity results were similar to those of the control test sample, therefore suggesting hemocompatibility of the tested materials.

Synthesis and in vitro cytotoxicity evaluation of ruthenium polypyridyl-sensitized paramagnetic titania nanoparticles for photodynamic therapy

RSC Advances ◽  
2016 ◽  
Vol 6 (53) ◽  
pp. 47520-47529 ◽  
Author(s):  
Mohammad H. Sakr ◽  
Najeeb M. Halabi ◽  
Leen N. Kalash ◽  
Sara I. Al-Ghadban ◽  
Mayyasa K. Rammah ◽  
...  
Keyword(s):  
A549 Cells ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Lung Cancer Cell Line ◽  
Titania Nanoparticles ◽  
Human Lung Cancer ◽  
Type I ◽  
Dye Sensitized ◽  
Photo Dynamic Therapy

We demonstrate the effective cytotoxic properties of a dye-sensitized metal oxide in an in vitro model of a human lung cancer cell line (A549 cells) upon light irradiation, where a type I mechanism photo-dynamic therapy is realized exclusively.

scholarly journals Antibacterial Activity and Cytotoxicity of Immobilized Glucosamine/Chondroitin Sulfate on Polylactic Acid Films

Polymers ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 1186 ◽  
Author(s):  
Ilkay Karakurt ◽  
Kadir Ozaltin ◽  
Daniela Vesela ◽  
Marian Lehocky ◽  
Petr Humpolíček ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Synergistic Effect ◽  
Chondroitin Sulfate ◽  
Polylactic Acid ◽  
Photoelectron Spectroscopy ◽  
Polymeric Materials ◽  
Bactericidal Effect ◽  
In Vitro Cytotoxicity ◽  
Major Drawback

Polylactic acid (PLA) is one of the most produced polymeric materials, due to its exceptional chemical and mechanical properties. Some of them, such as biodegradability and biocompatibility, make them attractive for biomedical applications. Conversely, the major drawback of PLA in the biomedical field is their vulnerability to bacterial contamination. This study focuses on the immobilization of saccharides onto the PLA surface by a multistep approach, with the aim of providing antibacterial features and evaluting the synergistic effect of these saccharides. In this approach, after poly (acrylic acid) (PAA) brushes attached non-covalently to the PLA surface via plasma post-irradiation grafting technique, immobilization of glucosamine (GlcN) and chondroitin sulfate (ChS) to the PAA brushes was carried out. To understand the changes in surface properties, such as chemical composition, surface topography and hydrophilicity, the untreated and treated PLA films were analyzed using various characterization techniques (contact angle, scanning electron microscopy, X-ray photoelectron spectroscopy). In vitro cytotoxicity assays were investigated by the methyl tetrazolium test. The antibacterial activity of the PLA samples was tested against Escherichia coli and Staphylococcus aureus bacteria strains. Plasma-treated films immobilized with ChS and GlcN, separately and in combination, demonstrated bactericidal effect against the both bacteria strains and also the results revealed that the combination has no synergistic effect on antibacterial action.

scholarly journals Preparation and evaluation of chitosan based thermoreversible gels for intraperitoneal delivery of 5-fluorouracil (5-FU)

2013 ◽  
Vol 63 (4) ◽  
pp. 479-491 ◽  
Author(s):  
Bhavesh P. Depani ◽  
Anuja A. Naik ◽  
Hema A. Nair
Keyword(s):  
Antineoplastic Agent ◽  
In Vitro Cytotoxicity ◽  
In Vivo Studies ◽  
Comparable Efficacy ◽  
Prolonged Release ◽  
Fibroblast Cells ◽  
Glycerol Phosphate ◽  
Drug Free

Abstract Sterile thermoreversibly gelling systems based on chitosan- glycerol phosphate were developed for intraperitoneal delivery of the antineoplastic agent 5-FU. The formulation was evaluated for gelling characteristics and in vitro drug release. Drug free gels were evaluated for in vitro cytotoxicity in L-929 mouse fibroblast cells. Drug loaded gels were subjected to acute toxicity studies in Swiss albino mice via intraperitoneal route and efficacy studies via intratumoral injections in subcutaneous colon carcinoma bearing BALB/c mice. The formulations gelled reversibly in 8 min at 37 °C and provided prolonged release of the drug. Drug free systems showed dose dependent cytotoxicity in fibroblast cells, while in vivo studies revealed a 2.8-fold increase in LD50 of 5-FU administered intraperitoneally as the developed system. Tumor volume measurements showed comparable efficacy of 5-FU administered as gel and commercial injection with a greatly improved safety profile of the former as adjudged from mortality and body weight measurements.

scholarly journals Formulation and in-vitro evaluation of ciprofloxacin HCL floating matrix tablets

2020 ◽  
Vol 2 (1) ◽  
pp. 01-06
Author(s):  
Dhulipalla Mounika ◽  
I. Deepika Reddy ◽  
K. Sai Chandralekha ◽  
Kapu Harika ◽  
Ramarao Nadendla ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Release ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Prolonged Release ◽  
Evaluation Parameters

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared.

In vitro cytotoxicity investigations of chloroform extract of Anisomeles malabarica on vero and lung cancer [A-549] cell lines

2021 ◽  
Vol 16 (12) ◽  
pp. 95-99
Author(s):  
Duguluri Sajusha ◽  
Sivagnanam Selvakumar
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Human Lung ◽  
Chloroform Extract ◽  
In Vitro Cytotoxicity ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Thiazolyl Blue Tetrazolium Bromide ◽  
Thiazolyl Blue Tetrazolium

The main objective of this study is to investigate the cytotoxic potential of chloroform extract of medicinal plant Anisomeles malabarica. Successive solvent extraction of Anisomeles malabarica in chloroform was done. The extracts were tested against normal cell lines (Vero) human lung cancer cell lines (A-549) using the thiazolyl blue tetrazolium bromide test (MTT) assay. The results of the present investigation revealed that the chloroform extract of Anisomeles malabarica shown anti-lung cancer activity. The evaluation of the toxicity of medicinal plants and their herbal preparations is essential to determine the applicability of the samples as pharmacological drugs. Further studies are necessary for more extensive pharmacological and toxicological evaluations.

Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities

2017 ◽  
Vol 96 ◽  
pp. 232-242 ◽  
Author(s):  
Elham Abdelmonem Mohamed ◽  
Irhan Ibrahim Abu Hashim ◽  
Rehab Mohammad Yusif ◽  
Ghada Mohamed Suddek ◽  
Ahmed Abdel Aziz Shaaban ◽  
...  
Keyword(s):  
In Vitro Cytotoxicity ◽  
Prolonged Release ◽  
Anti Tumor Activity

Development of Gold-Coated Magnetic Nanoparticles as a Potential MRI Contrast Agent

NANO ◽  
2015 ◽  
Vol 10 (04) ◽  
pp. 1550048 ◽  
Author(s):  
Ali Reza Montazerabadi ◽  
Mohammad Ali Oghabian ◽  
Rasoul Irajirad ◽  
Samad Muhammadnejad ◽  
Davoud Ahmadvand ◽  
...  
Keyword(s):  
Contrast Agent ◽  
Early Stage ◽  
Superparamagnetic Iron Oxide ◽  
In Vitro Cytotoxicity ◽  
Mri Contrast Agent ◽  
Core Shell ◽  
Mri Contrast ◽  
Shell Particles

Gold-coated superparamagnetic iron oxide nanoparticles (SPIONs) coated with methyl-polyethylene glycol (mPEG) are synthesized and investigated as a magnetic resonance (MR) imaging contrast agent. The synthesized mPEG-core@shells are characterized by UV-visible spectroscopy, transmission electron microscopy (TEM), dynamic light scattering (DLS), vibrating sample magnetometry (VSM), zeta-potential analysis and X-ray diffraction (XRD). In addition, the transverse relaxivity of the mPEG-core@shells is measured using a 3 T MRI scanner. The cytotoxicity of the mPEG-core@shells is tested in the LNCaP cell line using an 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results show that the mPEG-core@shell particles are semispherical with hydrodynamic size of ∼ 65 nm and a transverse relaxivity of 162.3 mM-1 S-1. The mPEG-core@shell particles demonstrate good stability in biological media without any significant in vitro cytotoxicity under high cellular uptake conditions. Finally, in vivo imaging shows that mPEG-core@shells are a potential contrast agent for use in early-stage detection.

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